Preparation of avermectin medicament sustained-release nano microsphere preparations and uses thereof

A technology of abamectin and nano-microspheres, applied in application, drug combination, animal repellent, etc., can solve the problems of large impact on soil ecological environment, low bioavailability, long residual time, etc., and achieve ecological benefits Effects of environment, bioavailability enhancement, and prolongation of drug efficacy

Inactive Publication Date: 2008-06-11
INST OF PLANT PROTECTION CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a pesticide, there are problems such as high toxicity, long residual effect time, great impact on the soil ecological environment, poor stability, low bioavailability, low efficiency, and high cost, which limit the large-scale application of this biological pesticide.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, in the there-necked flask that agitator, reflux condenser, thermometer are equipped with, the abamectin class medicine that contains 40%, 1% divinylbenzene (cross-linking agent), 1% BPO (initiator) The solution of methyl acrylate) was suspended at 40°C in the water phase containing 1% sodium dodecylbenzenesulfonate and 0.5% PVA (the volume ratio of the oil phase to the water phase was 1:3), and 1 ml 0.5% methylene blue. Adjust the ultrasonic power, after the size of the liquid beads is suitable and the particle size is uniform, raise the temperature to 61°C at a speed of 5°C / 10min, polymerize for 2 hours, then raise the temperature to 85°C at the same speed, and polymerize for 8 hours to obtain drugs with different drug loadings 50nm-100nm abamectin drug microsphere preparation.

Embodiment 2

[0029] Embodiment 2, in the there-necked flask that agitator, reflux condenser, thermometer are equipped with, the abamectin class medicine that contains 14%, 2.4% divinylbenzene (cross-linking agent), 1% BPO (initiator) The solution of methyl acrylate) was suspended at 40°C in an aqueous phase containing 1% sodium dodecylbenzenesulfonate and 0.5% gelatin (the volume ratio of the oil phase to the water phase was 1:3), and 2 ml 0.5% methylene blue. Adjust the ultrasonic power, after the size of the liquid beads is suitable and the particle size is uniform, raise the temperature to 61°C at a speed of 5°C / 10min, polymerize for 2 hours, then raise the temperature to 85°C at the same speed, and polymerize for 8 hours to obtain drugs with different drug loadings 50nm-100nm abamectin drug microsphere preparation.

Embodiment 3

[0030] Embodiment 3, in the there-necked flask that agitator, reflux condenser, thermometer are equipped with, the solution of the glycidyl methacrylate that contains 14% avermectins medicine, 1% BPO (initiator) is suspended in Add 1 ml of 0.5% methylene blue to the aqueous phase containing 1% sodium dodecylbenzenesulfonate and 0.5% PVA at 40°C (the volume ratio of the oil phase to the aqueous phase is 1:3). Adjust the ultrasonic power, after the size of the liquid beads is suitable and the particle size is uniform, raise the temperature to 61°C at a speed of 5°C / 10min, polymerize for 2 hours, then raise the temperature to 85°C at the same speed, and polymerize for 8 hours to obtain drugs with different drug loadings 50nm-100nm abamectin drug microsphere preparation.

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PUM

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Abstract

The invention relates to a process for preparing avermectin and derivant dimethylamino avermectin, ivermectin, and doramectin slow release nanometer micro-balloon preparation. The technical procedures comprise suspending the suspending solution of 1%-40% unequal avermectin-type medicine, 0%-4% divinylbenzene (cross linking agent), (metyl group) methyl acrylate of 1% BPO (initiating agent) or solvent of methacrylic acid glycidyl ester in an aqueous phase of 40 DEG C with 1% sodium dodecyl benzene sulfonate and 0.5% gelatine or 0.5% PVA (the size ratio of an oil phase and the aqueous phase is 1:3) in a three-mouth bottle with an agitator, a reflux condensing tube and a thermometer, adding numerous ml of 0.5% methylene blue, regulating ultrasonic homogenization power, heating-up to 61 DEG C at 5 DEG C/10mins after the grain size is even, aggregating for two hours, heating-up to 85 DEG C with the same speed, aggregating for 8 hours and preparing 50nm-100nm avermectin-type medicinal nanometer micro-balloon preparation with different medicine-loading amount, and the packaging and loading rate reaches more than 91%. The invention solves the problem of long-acting controlled release of biological medicament, reduces the toxic and side effect simultaneously, improves the biological availability, reduces the cost and is friendly to the environment.

Description

technical field [0001] The invention relates to a preparation method and application of abamectin and its derivatives emamectin, ivermectin and doramectin slow-release nano-microsphere preparations. technical background [0002] Avermectins are currently the most excellent class of broad-spectrum and high-efficiency insecticides, and are also the fastest growing and most widely used biomedicine and antiparasitic drugs in the world. However, as an in vivo drug, the effective blood drug concentration is only maintained for about 68 hours, and the bioavailability is only 20%-30%. As a pesticide, there are problems such as high toxicity, long residual effect time, great impact on the soil ecological environment, poor stability, low bioavailability, low efficiency, and high cost, which limit the large-scale application of this biological pesticide. Contents of the invention [0003] The purpose of the present invention is to address the disadvantages of the above-mentioned pri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/90A01N25/28A61K31/7048A61P33/14
Inventor 宁君梅向东黄啟良赵前飞李永红马洪菊杨国权宋倩张涛
Owner INST OF PLANT PROTECTION CHINESE ACAD OF AGRI SCI
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